The concept of “hybrid molecules” is an in-progress approach for the production of "newly evolved molecular species" where different pharmacophores (of currently available active ingredients) are linked, fused or merged to natural bioactive compounds. These “hybrids”, which identify a co-drug, a fused drug, a conjugate or a chimeric drug,1 often display therapeutic potential for multiple diseases. Naturally occurring polyphenols have been used to treat and prevent a variety of chronic pathologies, including cancer, diabetes, and inflammations.2 Thus, their use to achieve new drugs with beneficial health properties is grewing. In this context, gallic acid-based hybrids linked to other bioactive phenolic have been developed, thus obtaining anti-inflammatory agents with a gastroprotective effect.3 Resveratrol-based chimeric hybrids, combining the stilbenoids with different bioactive scaffolds, are excellent anticancer agents.4 Based on these findings, we have developed a strategy to synthesize a group of gallic acidresveratrol hybrid molecules (GA-Resv) as potential bioactive compounds (Figure 1). The synthesis of GA-Resv hybrid molecules is achieved through protection-condensationdeprotection steps. Whereas other hybrids related to resveratrol are obtained starting from eugenol, employing Grubbs catalyst for cross-metathesis, and other steps. The new molecules will be studied for their role against diabetes-related complications.

Synthesis of gallic acid-resveratrol hybrid molecules as potential bioactive compounds

Nunzio Cardullo
Primo
;
Claudia Sciacca;Vera Muccilli
Ultimo
2022-01-01

Abstract

The concept of “hybrid molecules” is an in-progress approach for the production of "newly evolved molecular species" where different pharmacophores (of currently available active ingredients) are linked, fused or merged to natural bioactive compounds. These “hybrids”, which identify a co-drug, a fused drug, a conjugate or a chimeric drug,1 often display therapeutic potential for multiple diseases. Naturally occurring polyphenols have been used to treat and prevent a variety of chronic pathologies, including cancer, diabetes, and inflammations.2 Thus, their use to achieve new drugs with beneficial health properties is grewing. In this context, gallic acid-based hybrids linked to other bioactive phenolic have been developed, thus obtaining anti-inflammatory agents with a gastroprotective effect.3 Resveratrol-based chimeric hybrids, combining the stilbenoids with different bioactive scaffolds, are excellent anticancer agents.4 Based on these findings, we have developed a strategy to synthesize a group of gallic acidresveratrol hybrid molecules (GA-Resv) as potential bioactive compounds (Figure 1). The synthesis of GA-Resv hybrid molecules is achieved through protection-condensationdeprotection steps. Whereas other hybrids related to resveratrol are obtained starting from eugenol, employing Grubbs catalyst for cross-metathesis, and other steps. The new molecules will be studied for their role against diabetes-related complications.
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/20.500.11769/549723
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